Adrenergic Drugs Flashcards
Amphetamine
Action: Release of catecholamines from nerve terminals; indirect-acting sympathomimetic.
Uses: ADHD; narcolepsy; abuse/addiction.
Toxicity: Hypertension; MI; stroke; priapism.
Cocaine
Action: Blocks reuptake of catecholamines into nerve terminals.
Uses: Topical nasal anesthesia; nasal bleeding.
Toxicity: Tachycardia; vasoconstriction; arrhythmia; angina; vasoconstriction; hallucinations; mydriasis.
Other: Has local anesthetic action independent of its actions on catecholamine transporter.
Ephedrine
Action: Mixed-acting sympathomimetic; increases the activity of NE at adrenergic receptos.
Uses: Acute bronchcospasm; anesthesia-related hypotension; OTC nasal decongestant.
Toxicity: Tachycardia; arrhythmia; hypertension.
Other: Contraindicated in closed-angle glaucoma and BPH.
Imipramine
Action: Tricyclic anti-depressant; inhibits catecholamine uptake into nerve terminal.
Uses: Depression.
Toxicity: Tachycardia; constipation; urinary retention; disorientation.
Other: Also acts as a muscarinic receptor antagonist.
Alpha-methyl tyrosine (metyrosine)
Action: Inhibits tyrosine hydroxylase (inhibition of DOPA production).
Uses: Pheochromocytoma.
Toxicity: Diarrhea; anxiety; hallucinations.
Alpha-methyldopa
Action: Converted to alpha-methyl-norepinephrine, which acts as a central alpha-2-adrenergic agonist; decreases sympathetic outflow.
Uses: Hypertension.
Toxicity: Orthostatic hypotension; bradycardia; sedation; headache.
Reserpine
Action: Inhibits vesicular monoamine transporter (VMAT) and prevents loading of DOPA into presynaptic vesicles; reduces NE release.
Uses: Hypertension; antipsychotic.
Toxicity: Arrhythmia; bradycardia; sexual dysfunction; headache; depression.
Tranylcypromine
Action: MAO inhibitor.
Uses: Depression.
Toxicity: Hypotension; sexual dysfunction; increased risk of suicide.
Other: Hypertensive crisis if consume foods high in tyramine.
Albuterol
Action: Beta-2-adrenergic agonist.
Uses: Bronchospasm.
Other: Also available combined with ipratropium (Combivent®).
Clonidine
Action: Selective alpha-2-adrenergic agonist (CNS acting).
Uses: Hypertension; ADHD.
Toxicity: Hypotension; bradycardia; sexual dysfunction.
Other: Acts in the CNS to decrease sympathetic outflow.
Dobutamine
Action: Selective beta-1-adrenergic agonist (also has some alpha-1-adrenergic agonist activity).
Uses: Increase cardiac output.
Toxicity: Tachycardia; hypertension.
Other: Low doses preferentially increase force over rate of contraction of heart; higher doses increase both and used for stress tests.
Dopamine
Uses: Agonist at dopamine, beta-adrenergic , and alpha-1-adrenergic recceptors.
Uses: Shock (especially w/ renal shutdown); heart failure; bradycardia.
Toxicity: Tachycardia; vasoconconstriction; local necrosis.
Epinephrine
Action: Adrenergic receptor agonist.
Uses: Anaphylaxis; bronchospasm; cardiac arrest.
Toxicity: Anxiety; arrhythmia; nausea; local necrosis.
Other: Produces mydriasis; preferentially binds beta-2 at low doses (decreased vascular resistance); binds beta-2 and alpha-1 at high doses (increased vascular resistance).
Fenoldopam
Action: Selective D1-dopamine receptor agonist; vasodilator of renal and mesenteric vasculature.
Uses: Severe hypertension.
Toxicity: Hypotension; tachycardia.
Other: Short-term IV administration for up to 48 hours.
Isoproterenol
Action: Non-selective beta-adrenergic receptor agonist.
Uses: Bradycardia; heart block; bronchospasm; hypoperfusion states.
Toxicity: Blurred vision; tachycardia; hypotension.
Midodrine
Action: Selective alpha-1-adrenergic receptor agonist.
Uses: Orthostatic hypotension.
Toxicity: Hypertension; bradycardia.
Mirabegron
Action: Selective beta-3-adrenergic agonist (~95% of beta receptors in bladder are B3).
Uses: Overactive bladder; urinary incontinence.
Toxicity: Tachycardia; hypertension.
Norepinephrine
Action: Adrenergic receptor agonist.
Uses: Restoration of blood pressure in acute hypotensive states; adjunctive treatment in cardiac arrest.
Toxicity: Arrhythmia; hypertension; bradycardia; extravasation necrosis.
Other: Pharmacologically administered NE not effective at beta-2-adrenergic receptors.
Phenylephrine
Action: Alpha-adrenergic receptor agonist.
Uses: Nasal congestion.
Toxicity: Hypertension; bradycardia; CNS stimulation; headache; urinary retention.
Salmeterol
Action: Long-acting selective beta-2-adrenergic receptor agonist.
Uses: Asthma; exercise-induced bronchospasm; COPD.
Toxicity: Paradoxical bronchospasm and asthma-related death; tachycardia; arrhythmia.
Other: Contraindicated without concomitant long-term asthma control medication (available combined with fluticasone, i.e. Advair®).
Terbutaline
Action: Selective beta-2-adrenergic receptor agonist.
Uses: Bronchospasm; premature labor.
Toxicity: Tachycardia.
Atenolol
Action: Selective beta-1-adrenergic receptor antagonist.
Uses: Hypertension; angina; myocardial infarction; migraine prophylaxis.
Other: Risk of MI and angina if abrupt cessation of treatment.
Carvedelol
Action: Both selective alpha-1- and non-selective beta-adrenergic antagonist.
Usage: Hypertension; congestive heart failure.
Toxicity: Bradycardia; heart block; bronchoconstriction.
Other: Risk of MI and angina if abrupt cessation of treatment; alpha:beta blockade > 1:10; “biased agonist” at beta-1-receptor.
Labetalol
Action: Selective alpha-1- and non-selective beta-adrenergic antagonist.
Usage: Hypertension.
Toxicity: Bradycardia; heart block; bronchoconstriction; impaired ejaculation.
Other: Risk of MI and angina if abrupt cessation of treatment; alpha:beta blockade ~1:3- 1:7.
Metopralol
Action: Beta-1-adrenergic receptor antagonist.
Usage: Hypertension; angina; CHF.
Toxicity: Bradycardia; bronchospasm.
Other: Risk of MI and angina if abrupt cessation of treatment.
Mirtazapine
Action: Selective alpha-2-adrenergic antagonist; also 5-HT2 antagonist (seratonin receptors).
Usage: Depression.
Toxicity: Abnormal thinking and dreams; arrhythmia.
Other: Increases risk of suicide…hmmmm.
Nadolol
Action: Non-selective beta-adrenergic receptor antagonist.
Usage: Hypertension; angina; ventricular arrhythmia; vascular and migraine headache prophylaxis.
Toxicity: Bradycardia; arrhythmia; bronchospasm.
Other: Risk of MI and angina if abrupt cessation of treatment; relatively long-acting.
Phenoxybenzamine
Action: Covalent (long-acting) alpha-adrenergic antagonist.
Usage: Pheochromocytoma (treatment).
Toxicity: Orthostatic (positional) hypotension; tachycardia; miosis; sexual dysfunction; nasal congestion.
Other: Alkylates the alpha-adrenergic receptor; causes “non-equilibrium blockade”.
Phentolamine
Action: Reversible (short-acting) alpha-adrenergic antagonist.
Usage: Dx of pheochromocytoma; extravasation necrosis; reversal of local dental anasthesia.
Toxicities: Orthstatic hypotension; tachycardia; nasal congestion; diarrhea.
Other: Short acting (as opposed to phenoxybenzamine).
Prazosin
Action: Alpha-1-adrenergic antagonist.
Usage: Hypertension; BPH (relax sphincters).
Toxicities: Orthostatic hypotension.
Other: Less tachycardia than nonselective antagonists.
Propanolol
Action: Non-selective beta-adrenergic receptor antagonist.
Usage: Hypertension; angina; congestive heart failure; arrhythmia; essential tremor; migraine.
Toxicities: Bradycardia; bronchoconstriction; heart block; depression/sedation.
Other: Risk of MI and angina if abrupt cessation of treatment.
Tamsulosin
Action: Selective alpha-1A- and alpha-1D-adrenergic receptor antagonist.
Usage: Benign prostatic hyperplasia.
Toxicities: Orthostatic hypotension; decreased libido.
Other: Also used to facilitate expulsion of kidney stones; tradename Flomax.
Timolol
Action: Non-selective beta-adrenergic receptor antagonist.
Usage: Hypertension; angina; post-MI CV event prevention; migraine prophylaxis; glaucoma.
Toxicity: Bradycardia; bronchospasm; headache; impotence.
Other: Risk of MI and angina if abrupt cessation of treatment.
